MIM1

MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 uM) that overcomes Mcl-1-dependent leukemia cell survival.

IC50 value: 4.8 uM

Target: Mcl-1

MIM1 effectively competed with FITC-MCL-1 SAHBA and FITC-BID BH3 for MCL-1ΔNΔC binding with respective IC50s of 4.7 and 4.8 μM, the compound showed no capacity to displace FITC-BID BH3 from BCL-XLΔC (IC50>50 μM), mirroring the selectivity of MCL-1 SAHBD.

Although MCL-1 SAHBD was a 30 to 60-fold more potent competitor for MCL-1ΔNΔC binding than MIM1, the MCL-1 selective small molecule is one-seventh the size of the stapled peptide and exhibits an IC50 for its target (4.8 μM) that is only 7.5-fold less than that of chemically-optimized ABT-737 for BCL-XLΔC (0.63 μM) upon competition with FITC-BID BH3.